JP5496899B2 - シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン - Google Patents
シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン Download PDFInfo
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- JP5496899B2 JP5496899B2 JP2010530110A JP2010530110A JP5496899B2 JP 5496899 B2 JP5496899 B2 JP 5496899B2 JP 2010530110 A JP2010530110 A JP 2010530110A JP 2010530110 A JP2010530110 A JP 2010530110A JP 5496899 B2 JP5496899 B2 JP 5496899B2
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- cancer
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- 0 *[C@](C(N(CCC(N1)O)C1=O)O[C@]1CO)[C@]1O Chemical compound *[C@](C(N(CCC(N1)O)C1=O)O[C@]1CO)[C@]1O 0.000 description 2
- YYKPWSPWWHZLTO-JPCDQAEASA-N CC([C@@H]1F)O[C@H](CO)[C@H]1O Chemical compound CC([C@@H]1F)O[C@H](CO)[C@H]1O YYKPWSPWWHZLTO-JPCDQAEASA-N 0.000 description 1
- OIVLITBTBDPEFK-UHFFFAOYSA-N O=C(CCN1)NC1=O Chemical compound O=C(CCN1)NC1=O OIVLITBTBDPEFK-UHFFFAOYSA-N 0.000 description 1
- XOQSIJJEPLQOPY-KDBQFOGNSA-N OC(C1)C1([C@H]1O)OC(CN(CC[C@@H](N2)O)C2=O)[C@@H]1F Chemical compound OC(C1)C1([C@H]1O)OC(CN(CC[C@@H](N2)O)C2=O)[C@@H]1F XOQSIJJEPLQOPY-KDBQFOGNSA-N 0.000 description 1
- DINLEAHFNSLTEA-XDTPYFJJSA-N OC[C@H]([C@H]([C@H]1F)O)OC1N(CCCN1)C1=O Chemical compound OC[C@H]([C@H]([C@H]1F)O)OC1N(CCCN1)C1=O DINLEAHFNSLTEA-XDTPYFJJSA-N 0.000 description 1
- RTGAEUWOUHUIHP-FMDGEEDCSA-N OC[C@H]([C@H]([C@H]1F)O)O[C@H]1N(CC[C@H](N1)O)C1=O Chemical compound OC[C@H]([C@H]([C@H]1F)O)O[C@H]1N(CC[C@H](N1)O)C1=O RTGAEUWOUHUIHP-FMDGEEDCSA-N 0.000 description 1
- BUUQDDOATLEQQW-XVKVHKPRSA-N O[C@@H]([C@H]1O)[C@@H](C=O)O[C@H]1N(CCC(N1)O)C1=O Chemical compound O[C@@H]([C@H]1O)[C@@H](C=O)O[C@H]1N(CCC(N1)O)C1=O BUUQDDOATLEQQW-XVKVHKPRSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/073—Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98039707P | 2007-10-16 | 2007-10-16 | |
| US60/980,397 | 2007-10-16 | ||
| PCT/US2008/080163 WO2009052287A1 (en) | 2007-10-16 | 2008-10-16 | 2 ' -flu0r0-2 ' -deoxytetrahydrouridines as cytidine deaminase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014043175A Division JP5859588B2 (ja) | 2007-10-16 | 2014-03-05 | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011500713A JP2011500713A (ja) | 2011-01-06 |
| JP2011500713A5 JP2011500713A5 (enExample) | 2011-12-01 |
| JP5496899B2 true JP5496899B2 (ja) | 2014-05-21 |
Family
ID=40251685
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010530110A Active JP5496899B2 (ja) | 2007-10-16 | 2008-10-16 | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
| JP2014043175A Active JP5859588B2 (ja) | 2007-10-16 | 2014-03-05 | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014043175A Active JP5859588B2 (ja) | 2007-10-16 | 2014-03-05 | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
Country Status (40)
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012522842A (ja) * | 2009-04-06 | 2012-09-27 | エーザイ インコーポレイテッド | シチジンベースの抗新生物薬とシチジンデアミナーゼ阻害薬との組合せ、および癌の治療におけるその使用 |
| JP2014177455A (ja) * | 2007-10-16 | 2014-09-25 | Eisai Inc | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11116782B2 (en) | 2002-10-15 | 2021-09-14 | Celgene Corporation | Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine |
| US8404716B2 (en) | 2002-10-15 | 2013-03-26 | Celgene Corporation | Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine |
| US7964580B2 (en) * | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
| HUE055911T2 (hu) | 2008-05-15 | 2021-12-28 | Celgene Corp | Citidin-analógokat tartalmazó orális készítmények, és eljárások azok alkalmazására |
| US8173621B2 (en) | 2008-06-11 | 2012-05-08 | Gilead Pharmasset Llc | Nucleoside cyclicphosphates |
| US20100055047A1 (en) * | 2008-08-26 | 2010-03-04 | Yiyu Zou | Methods for treating bronchial premalignancy and lung cancer |
| CL2009002206A1 (es) | 2008-12-23 | 2011-08-26 | Gilead Pharmasset Llc | Compuestos derivados de pirrolo -(2-3-d]-pirimidin-7(6h)-tetrahidrofuran-2-il fosfonamidato, composicion farmaceutica; y su uso en el tratamiento de enfermedades virales. |
| EP2417146B1 (en) * | 2009-04-06 | 2016-07-13 | Otsuka Pharmaceutical Co., Ltd. | (2'-deoxy-ribofuranosyl)-1,3,4,7-tetrahydro-(1,3)diazepin-2-one derivatives for treating cancer |
| WO2010118010A1 (en) * | 2009-04-06 | 2010-10-14 | Eisai Inc. | Combination of decitabine with cytidine deaminase inhibitor and use thereof in the treatment of cancer |
| US8609631B2 (en) | 2009-04-06 | 2013-12-17 | Eisai Inc. | Compositions and methods for treating cancer |
| GB0907551D0 (en) | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| TWI583692B (zh) | 2009-05-20 | 2017-05-21 | 基利法瑪席特有限責任公司 | 核苷磷醯胺 |
| US8618076B2 (en) | 2009-05-20 | 2013-12-31 | Gilead Pharmasset Llc | Nucleoside phosphoramidates |
| PL3290428T3 (pl) | 2010-03-31 | 2022-02-07 | Gilead Pharmasset Llc | Tabletka zawierająca krystaliczny (S)-2-(((S)-(((2R,3R,4R,5R)-5-(2,4-diokso-3,4-dihydropirymidyn-1(2H)-ylo)-4-fluoro-3-hydroksy-4-metylotetrahydrofuran-2-ylo)metoksy)(fenoksy)fosforylo)amino)propanian izopropylu |
| CL2011000716A1 (es) | 2010-03-31 | 2012-04-20 | Gilead Pharmasset Llc | Formas cristalinas 1 6 de (s)-isopropil-2-(((s)-(((2r.3r.4r.5r)-5-(2,4-dioxo-3,4-dihidropirimidin-1(2h)-il)-4-fluoro-3-hidroxi-4-metil tetrahidrofuran-2-il)metoxi)(fenoxi)fosforil)amino)propanoato; composicion y combinacion farmaceutica; y su uso para tratar una infeccion por el virus de la hepatitis c. |
| WO2012075140A1 (en) | 2010-11-30 | 2012-06-07 | Pharmasset, Inc. | Compounds |
| SI2709613T2 (sl) | 2011-09-16 | 2020-12-31 | Gilead Pharmasset LLC c/o Gilead Sciences, Inc. | Postopki za zdravljenje HCV |
| US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
| NZ729172A (en) | 2013-01-31 | 2018-06-29 | Gilead Pharmasset Llc | Combination formulation of two antiviral compounds |
| JP2016529293A (ja) | 2013-08-27 | 2016-09-23 | ギリアド ファーマセット エルエルシー | 2つの抗ウイルス化合物の組合せ製剤 |
| RU2681939C2 (ru) | 2013-10-29 | 2019-03-14 | Оцука Фармасьютикал Ко., Лтд. | Путь синтезирования 2'-дезокси-2'2'-дифтортетрагидроуридинов |
| JP6783224B2 (ja) | 2014-04-04 | 2020-11-11 | デル マー ファーマシューティカルズ | 肺の非小細胞癌腫及び卵巣癌を処置するためのジアンヒドロガラクチトール及びその類縁体又は誘導体の使用 |
| US10034872B2 (en) | 2014-08-22 | 2018-07-31 | Celgene Corporation | Methods of treating multiple myeloma with immunomodulatory compounds in combination with antibodies |
| CA3007357C (en) | 2015-12-03 | 2023-12-05 | Epidestiny, Inc. | Compositions containing decitabine, 5azacytidine and tetrahydrouridine and uses thereof |
| WO2017158396A1 (en) | 2016-03-16 | 2017-09-21 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Cytidine deaminase inhibitors for the treatment of pancreatic cancer |
| AU2019216531A1 (en) | 2018-02-02 | 2020-09-24 | Maverix Oncology, Inc. | Small molecule drug conjugates of gemcitabine monophosphate |
| WO2020047177A1 (en) * | 2018-08-28 | 2020-03-05 | Essenlix Corporation | Assay accuracy improvement |
| US11224610B2 (en) * | 2018-09-19 | 2022-01-18 | Otsuka Pharmaceutical Co., Ltd. | Low dose combination CDA substrate drug/cedazuridine with extended administration |
| CN112888700B (zh) * | 2018-10-19 | 2025-03-04 | 因特欧力多公司 | 具有改善治疗功效的修饰核酸和含有其的抗癌药物组合物 |
| WO2020080912A1 (ko) * | 2018-10-19 | 2020-04-23 | 인터올리고 주식회사 | 치료 효능을 개선한 핵산 변형체 및 이를 포함하는 항암용 약학 조성물 |
| US12187757B2 (en) * | 2019-10-08 | 2025-01-07 | Otsuka Pharmaceutical Co., Ltd. | 2′-deoxy-2′,2′-difluorotetrahydrouridines with high purity and methods of making the same |
| EP4069254B1 (en) * | 2020-02-25 | 2024-09-11 | Otsuka Pharmaceutical Co., Ltd. | Solid oral dosage forms comprising decitabine and cedazuridine |
| CN117835984A (zh) * | 2021-03-26 | 2024-04-05 | 克利夫兰诊所基金会 | 使用胞苷脱氨酶抑制剂治疗rna病毒感染 |
| WO2022254457A1 (en) * | 2021-05-29 | 2022-12-08 | Msn Laboratories Private Limited, R&D Center | An improved process for the preparation of (4r)-1-[(2r,4r,5r)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl) oxolan-2-yl]-4-hydroxy-1,3-diazinan-2one and its intermediate compounds |
| CN118354759A (zh) | 2021-10-19 | 2024-07-16 | 阿基拉比奥有限公司 | 包含2’-脱氧胞苷类似物的组合物及其用于治疗镰状细胞病、地中海贫血和癌症的用途 |
| WO2023076332A1 (en) * | 2021-11-01 | 2023-05-04 | St. John's University | Injectable liquid pharmaceutical compostion containing gemcitabine and a cytidine deaminase inhibitor |
| US20230271996A1 (en) * | 2021-12-25 | 2023-08-31 | Scinopharm Taiwan, Ltd. | Process for preparing cedazuridine |
| TW202410893A (zh) | 2022-08-31 | 2024-03-16 | 日商大塚製藥股份有限公司 | 用於治療t細胞淋巴瘤之結合治療 |
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| JP2014177455A (ja) * | 2007-10-16 | 2014-09-25 | Eisai Inc | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
| JP2012522842A (ja) * | 2009-04-06 | 2012-09-27 | エーザイ インコーポレイテッド | シチジンベースの抗新生物薬とシチジンデアミナーゼ阻害薬との組合せ、および癌の治療におけるその使用 |
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